title: A novel strategy for synthesis of 5-iodo ((125/131)I)-1, 2, 3-triazoles via click chemistry.
abstract: We report a facile and effective method for radioiodine-labeled radiopharmaceuticals via copper (I)-catalyzed click chemistry route. In the novel radioiodination method, 5-iodo ((125/131)I)-1, 2, 3-triazoles were synthesized after a 24-h click reaction in organic solvent with a radiochemical yield of 13%. However, in the aqueous phase, the radiochemical yield of the conjugation radioiodine to RGD via click chemistry was 0. This suggested an exchange between hydrogen ion and iodine ion in aqueous phase so that no enough radioiodine was left to conjugate with RGD. We propose different mechanisms of Cu (I)-catalyzed cycloaddition of organic azides and 1-iodo-alkynes in organic phase and aqueous phase.
authors.affiliation: PET-CT Center, Guangzhou General Hospital of Guangzhou Military Command, Guangzhou 510010, China. wangch628@163.com
authors.forename: Cheng
authors.initials: C
authors.lastname: Wang
authors.forename: Jilin
authors.initials: J
authors.lastname: Yin
authors.forename: Wei
authors.initials: W
authors.lastname: Zhou
authors.forename: Lan
authors.initials: L
authors.lastname: Zhang
authors.forename: Zheng
authors.initials: Z
authors.lastname: Zhou
mesh_terms: D057930:Click Chemistry; D007457:Iodine Radioisotopes; D019275:Radiopharmaceuticals / Q000138:chemical synthesis; D014230:Triazoles / Q000138:chemical synthesis*
chemical_list: D007457:Iodine Radioisotopes; D019275:Radiopharmaceuticals; D014230:Triazoles